Abstract |
CW-270033, an injectable carbapenem, is a novel, synthesized pyrrolidinyl-thio carbapenem. In the present study, the in-vitro and in-vivo antibacterial activities of CW-270033 against wild-type strains and clinical isolates were compared with those of imipenem and meropenem. CW-270033 was more active than imipenem against Gram-negative (Escherichia coli and Pseudomonas aeruginosa) clinical isolates, but was slightly less active than meropenem. Against the Gram-positive clinical isolates methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant Enterococcus (VRE), CW-270033 was slightly more active than meropenem, but was less active than imipenem. CW-270033 displayed potent in-vivo activity against E. coli ATCC 25922, P. aeruginosa ATCC 27853, and S. aureus SMITH in the mouse systemic infection model; the efficacy of CW-270033 in this model was 2--7 fold higher than that of meropenem. This activity was comparable to the in-vitro activity of CW-270033. An intravenous injection of CW-270033 showed that the half-life of CW-270033 in serum in mice was about 20 min, which was about two times that of meropenem. CW-270033 was also found to be resistant to hydrolysis by the mouse renal dehydropeptidase I (DHP-I) enzyme.
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Authors | JongMyeung Kim, Jong Ryul Ha, Se Woong Oh, Hong Gi Kim, Jin-Man Lee, Dong Gun Lee, Sang-Han Lee, Jong Guk Kim |
Journal | Biological & pharmaceutical bulletin
(Biol Pharm Bull)
Vol. 30
Issue 3
Pg. 575-9
(Mar 2007)
ISSN: 0918-6158 [Print] Japan |
PMID | 17329859
(Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
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Chemical References |
- Anti-Bacterial Agents
- CW-270033
- Carbapenems
- Protease Inhibitors
- Pyrrolidines
- Thienamycins
- Cilastatin
- Meropenem
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Topics |
- Animals
- Anti-Bacterial Agents
(administration & dosage, chemistry, pharmacology)
- Bacteria
(drug effects, growth & development)
- Bacterial Infections
(microbiology, prevention & control)
- Carbapenems
(administration & dosage, chemistry, pharmacology)
- Cilastatin
(administration & dosage, chemistry, pharmacology)
- Dose-Response Relationship, Drug
- Enterococcus faecalis
(drug effects, growth & development)
- Escherichia coli
(drug effects, growth & development)
- Injections, Intravenous
- Meropenem
- Methicillin Resistance
- Mice
- Microbial Sensitivity Tests
- Molecular Structure
- Protease Inhibitors
(administration & dosage, chemistry, pharmacology)
- Pseudomonas aeruginosa
(drug effects, growth & development)
- Pyrrolidines
(administration & dosage, chemistry, pharmacology)
- Staphylococcus aureus
(drug effects, growth & development)
- Thienamycins
(administration & dosage, pharmacology)
- Vancomycin Resistance
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